WHI-P131 - CAS:202475-60-3 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	WHI-P131
英文名称:	WHI-P131
别名:	WHI-P131 WHI P131;Janex 1;4-[(6,7-dimethoxy-4-quinazolinyl)amino]-phenol
CAS No:	202475-60-3	分子式:	C₁₆H₁₅N₃O₃	分子量:	297.31
CAS No:	202475-60-3
分子式:	C₁₆H₁₅N₃O₃
分子量:	297.31

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

W10025 WHI-P131 ≥98%(HPLC) (psaitong)

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包装规格：

5mg?25mg?50mg?in?glass?bottle

溶解性：

溶于DMSO

产品描述：

基本信息

产品编号：	W10025
产品名称：	WHI-P131
CAS:	202475-60-3	储存条件	粉末	-20℃	四年

分子式：	C16H15N3O3		溶于液体	-80℃	6个月
分子量：	297.31			-20℃	1个月
化学名：	4-[(6,7-dimethoxy-4-quinazolinyl)amino]-phenol
Solubility (25°C)：
体外:	DMSO	5mg/mL (16.81mM)
	Ethanol	Insoluble
	Water	Insoluble
体内(现配现用):
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	3.3635mL	16.8175mL	33.6349mL
5mM	0.6727mL	3.3635mL	6.7270mL
10mM	0.3363mL	1.6817mL	3.3635mL

生物活性

产品描述	一种有效的特异性JAK3抑制剂，Ki:2.3μM，IC50:78μM，WHI-P131不抑制JAK1和JAK2。
靶点	JAK3 (Cell-free assay)
靶点	78μM
体外研究	JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 of 78μM),does not inhibit JAK1 and JAK2,the ZAP/SYK family tyrosine kinase SYK,the TEC family tyrosine kinase BTK,the SRC family tyrosine kinase LYN,or the receptor family tyrosine kinase insulin receptor kinase,even at concentrations as high as 350μM.JANEX-1 induces apoptosis in JAK3-expressing human leukemia cell lines NALM-6 and LC1;19 but not in melanoma (M24-MET) or squamous carcinoma (SQ20B) cells.WHI-P131 inhibits the clonogenic growth of JAK3-positive leukemia cell lines DAUDI,RAMOS,LC1;19,NALM-6,MOLT-3,and HL-60 (but not JAK3-negative BT-20 breast cancer,M24-MET melanoma,or SQ20B squamous carcinoma cell lines) in a concentration-dependent fashion.WHI-P131 inhibits clonogenic growth in a concentration-dependent fashion with EC50s of 24.4μM for NALM-6 cells and 18.8μM for DAUDI cells. At 100μM,WHI-P131 inhibits the in vitro colony formation by these leukemia cell lines by >99%.In contrast,JANEX-1 does not inhibit the clonogenic growth of JAK3-negative M24-MET melanoma or SQ20B squamous carcinoma cell lines.
体内研究	JANEX-1 is administered at doses ranging from 5 to 100mg/kg.Evaluation of CPK activity revealed a dose-response curve with an effective dose 50 (ED50) value of 7.44mg/kg.Mice receiving JANEX-1 displayed significantly reduced CPK and LDH levels.In addition,the infarct size of JANEX-1-treated mice (30.16±2.79%) is significantly decreased when compared with I/Roperated mice (65.64±3.76%).JANEX-1 (WHI-P131) is absorbed rapidly, and the time to reach the maximum plasma JANEX-1 concentration (tmax) is 24.7±1.7 min.JANEX-1 is rapidly eliminated with an elimination half-life of 45.6±5.5 min.Although the predicted maximum plasma JANEX-1 concentration is 10.5±0.8μM,which is only half of the Cmax following i.v.administration of the same bolus dose,the i.p.bioavailability is 94.6% and the systemic exposure levels (i.e.,AUC) are very similar to those observed after i.v. injection (17.1±2.2μM•h versus 18.1±1.2μM•h).

推荐实验方法(仅供参考)

细胞实验:

The following cell lines are used in various biological assays:NALM-6 (pre-B-ALL),LC1;19 (pre-B-ALL),DAUDI (B-ALL),RAMOS (B-ALL),MOLT-3 (T-cell ALL),HL60 (acute myelogenous leukemia),BT-20 (breast cancer),M24-MET (melanoma),SQ20B (squamous cell carcinoma),and PC3 (prostate cancer).These cell lines are maintained in culture.Cells are seeded in six-well tissue culture plates at a density of 50×104 cells/well in a treatment medium containing various concentrations of JANEX-1 (0.1,0.2,0.3,0.4 and 0.5nM) and incubated for 24-48 h at 37℃ in a humidified 5% CO2 atmosphere. Cells are examined for apoptotic changes after treatment with JANEX-1 by the in situ TdT-mediated dUTP end-labeling assay using the ApopTag apoptosis detection kit.

动物实验:

Mice

Pathogen-free 8-week-old male JAK3-/-(129S4-Jak3tm1Ljb) and C57BL/6 J mice are used.Mice are treated with JANEX-1 at a dose of 20mg/kg (intraperitoneally) at 1h before ischemia.

Rats

Male Lewis rats are divided into two experimental groups of five and are injected either i.v.via the dorsal vein of the penis or i.p.with a single 3.3mg/kg bolus dose of JANEX-1.The rats are anesthetized by the methoxyfluran, and blood samples (0.2mL) are collected from rat tail vein before and at 5,10,and 30 min and 1,1.5,2,3,4,and 6h after i.v.injections or at 5,10,15,30,and 45 min and 1,1.5,2,3,4,5,and 7h after i.p.injections.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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